Abstract: The present invention provides a process for catalytically hydrogenating unsaturated phytosterol compounds. The catalyst used for such hydrogenation is an alumina-supported transition metal selected from the group consisting of nickel, palladium, platinum, ruthenium, rhodium and mixtures thereof. The process involves the following steps.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: A cationic amphiphile for facilitating transport of a biologically active molecule into a cell has the structure A-F-D, in which A is a lipid anchor, D is a head group, and F is a spacer group having the structure described herein. A method for facilitating transport of a biologically active molecule into a cell comprises preparing a lipid mixture comprising a cationic amphiphile having structure A-F-D, preparing a lipoplex by contacting the lipid mixture with a biologically active molecule; and contacting the lipoplex with a cell, thereby facilitating transport of the biologically active molecule into the cell.

Abstract: The invention relates to a method for representing compounds of the general formula (1). The invention further relates to the hitherto unknown compounds of general formulas (5, 6 and 7) in the form of intermediate products and to the use of 4,4-dimethyl-3&bgr; hydroxypregna-8,14-diene-21-carboxylic acid esters of the general formula (1) for producing 4,4-dimethyl-5&agr;-cholesta-8,14,24-triene-3&bgr;-ol (2).

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids, does not produce or use non-food grade products and is substantially free of the use of a catalyst.

Abstract: The invention relates to a process for isolating sterols and tocopherols from mixtures of fats and fatty derivatives and from residues left after they have been worked up. After splitting of the glycerides by hydrolysis and subsequent removal of the free fatty acids by distillation, the sterol esters still present are largely split into free sterols by an additional hydrolysis step.

Abstract: A process for treating human skin by inhibiting serine protease formation involving contacting the skin with a composition containing a sterol sulfate.

Abstract: This invention relates to phytosterols and phytostanols, in particular to fatty acid esters of phytosterols and phytostanols with a specified fatty acid composition. The invention further relates to methods for preparation of the phytosterol and phytostanol esters and their uses.

Abstract: The present invention is directed to improved processes for phosphorylation and compounds produced by the improved processes. The improved process for phosphorylating complex alcohols comprises the following steps: (a) forming an intimate mixture of one or more complex alcohols and P4O10 at a temperature below 80° C. in the absence of additional solvents; and (b) allowing the intimate mixture to continue to react for a period of time at a temperature below 80° C. until the formation of the dihydrogen form of the phosphorylated complex alcohol is substantially completed.

Abstract: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.

Abstract: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.

Abstract: The present invention provides novel carbamate-based cationic lipids of the general structure: 1

Abstract: Olive oil based products, based on the virgin olive oils, containing plant stanol and/or sterol fatty acid ester blends and methods for preparing such olive oil based products.

Abstract: According to the present invention, it is possible to produce emulsions containing a material that are insoluble or that have low solubility with respect to water and oil in a high concentration, so as to obtain emulsions which can be preserved for a long period of time. More specifically, ethanol, to which polyglycerol oleic acid ester (PG) is added, and vegetable oil, are stirred with a homogenizer or an emulsification method such as a membrane emulsification or a microchannel emulsification, thereby obtaining E/O type emulsions or E/O/W type emulsions wherein ethanol drops in which polyphenol is dissolved in a high concentration are dispersed into vegetable oil.

Abstract: Conjugates of a hydrophobic moiety, such as a lipid, linked through a cleavable dithiobenzyl linkage to a therapeutic agent are described. The dithiobenzyl linkage is susceptible to cleavage by mild thiolysis, resulting in release of the therapeutic agent in its original form. The linkage is stable under nonreducing conditions. The conjugate can be incorporated into liposomes for administration in vivo and release of the therapeutic agent in response to endogeneous in vivo reducing conditions or in response to administration of an exogeneous reducing agent.

Abstract: The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03H or ═NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; R4 is hydrogen, (C1-6)alkyl or (C1-6)acyl; R5 is hydrogen; or R5 designates, together with R6, an additional bond between the carbon atoms at which R5 and R6 are placed; R6 is hydrogen, hydroxy or halogen; or R6 designates, together with R5, an additional bond between the carbon atoms at which R6 and R5 are placed; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, optionally substituted with OH, (C1-4)alkoxy, or halogen; or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.

Abstract: The invention concerns hydrogenated phenanthrenes of formula I wherein the parameters have the meanings given in the text and their use in liquid crystal compositions.

Abstract: A cationic lipid useful in transfection of cells with DNA is disclosed.

Abstract: This invention relates to the field of estrogen receptors and particularly though not exclusively on the effect of estrogen receptors and ligands for estrogen receptors on the prevention or treatment of obesity. The invention also relates to the effect of estrogen receptors and their ligands on lipoprotein levels in mammals.

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids, does not produce or use non-food grade products and is substantially free of the use of a catalyst.

Abstract: A food additive useful for lowering serum cholesterol in humans contains a sterol or stanol ester of a fatty acid or a dicarboxylic acid ester of a sterol or stanol made by reacting a sterol, stanol and a carboxylic acid in the presence of an effective amount of a catalyst selected from the group consisting of calcium oxide, calcium hydroxide, a calcium salt of a carboxylic acid, magnesium hydroxide and combinations thereof described herein below.

Abstract: The invention relates to compounds with the general formula Y1—A1—M1—A2—Y2 wherein Y1 and Y2 are different from each other and Y1 is an acrylate or methacrylate residue and Y2 is a vinyl ether, epoxy, or azide residue, A1 and A2 are identical or different residues with the general formula CnH2n in which n is a whole number from 0 to 20 and one or more methylene groups can be replaced by oxygen atoms, and M1 has the general formula —R1—X1—R2—X2—R3—X3—R4— wherein R1, R2, R3, and R4 are identical or different doubly bonded residues from the group —O—, —COO—, —CONH—, —CO—, —S—, —C≡C—, —CH═CH—, —CH═N—, —CH2—, —N═N—, and —N═N(O)—, and R2—X2—R3 can also be a C—C bond, and X1, X2, and X3 are identical or different residues from the group 1,4-phenylene, 1,4-cyclohexylen

Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process for

Abstract: Novel sterol/stanol esters of a conjugated fatty acid are provided through the esterification or transesterification of a sterol such as beta-sitosterol or a hydrogenated form thereof (stanol). Such novel esters exhibit the combined properties normally possess by the sterol/stanol compound and the conjugated fatty acid and as such are excellent additives for dietetic foods and supplements.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids, does not produce or use non-food grade products and is substantially free of the use of a catalyst.

Abstract: The invention concerns concentrates of shea sterols in glycerides with more than 12.5 wt % shea sterols, the preparation thereof by enzymic hydrolysis of glycerides in shea oils or fractions thereof and the application of the concentrates in aerated food products.

Abstract: The present invention relates to novel carborane cholesterol analogs and their use in the treatment of tumor and cancers in humans, and in particular to the treatment of human brain tumors. Pharmaceutical compositions and methods of using these compositions in the treatment of tumors and cancer are other aspects of the present invention.

Abstract: Plant sterols have been shown to be cholesterol-reducing agents in human serum. In the present invention, plant sterols, plant stanols, plant sterol esters and other non-toxic sterols are micromilled with emulsifiers in a solvent (water or edible oil) to produce dispersion which can be incorporated into full-fat, reduced-fat, low-fat, fat-free and triglyceride-free food products. Such water-based or edible oil-based dispersions can be used to incorporate relatively high levels of such sterols/stanols in food products without the adverse organoleptic effect normally associated with the use of such plant sterols and plant stanols.

Abstract: The invention provides methods for separating outer birch bark from inner birch bark. The invention also provides methods for isolating betulin; lupeol; betulinic acid; 9,10-epoxy-18-hydroxyoctadecanoic acid; 9,10,18-trihydroxyoctadecanoic acid; polyphenolic polymers and fatty acids from birch bark.

Abstract: The invention relates to a process for the production of sterols from fatty acid distillation residues, characterized in that the partial glycerides are subjected to a first transesterification step under mild conditions and, after working up and the removal of impurities, the sterol esters are subjected to a second transesterification step under more extreme conditions.

Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.

Abstract: The present invention relates to novel retinol derivatives having the formula (I): and to processes for preparing them. The invention also relates to the use of these compounds in or for the preparation of compositions intended for treating conditions of the skin or scalp, for example in preventing or combating acne and/or chronological or actinic ageing of the skin.

Abstract: The invention relates to a process for the preparation of stanol esters by hydrogenating a sterol blend in a hydrogenation solvent and at an elevated temperature in the presence of a hydrogenation catalyst, by removing the hydrogenation catalyst from the obtained hot reaction solution, by transesterifying the intermediate stanol blend with a fatty acid methyl ester at an elevated temperature and in the presence of a transesterification catalyst, and by finally purifying the stanol ester blend thus obtained. According to the invention, the intermediate stanol blend is neither crystallized nor removed from the reaction solution but the hydrogenation solvent is replaced therein at least in part by a transesterification reagent. Alternatively, the hydrogenation solvent may also be used as the transesterification solvent, and preferably also as the transesterification reagent.

Abstract: Provided is a method for preparing a true, homogeneous solution of a pharmaceutical substance dissolved in an organic solvent in which the pharmaceutical substance is not normally soluble. Solubilization is obtained by forming a hydrophobic ion pair complex involving the pharmaceutical substance and an amphiphilic material. The resulting organic solution may be further processed to prepare pharmaceutical powders. A biodegradable polymer may be co-dissolved with the pharmaceutical substance and the amphiphilic material and may be incorporated into a pharmaceutical powder. A preferred method for preparing pharmaceutical powders is to subject the organic solution to gas antisolvent precipitation using a supercritical gas antisolvent such as carbon dioxide. Also provided is a method for making hollow particles having a fiber-like shape which would provide enhanced retention time in the stomach if ingested by a human or animal host.

Abstract: The invention relates to the use of nanoscale sterols and/or sterol esters with particle diameters of 10 to 300 nm as food additives and as active substances for the production of hypocholesterolemic agents. The particular fineness of the particles promotes more rapid absorption by the blood serum after oral ingestion by comparison with conventional sterols and sterol esters.

Abstract: A compound having the general formula: 1

Abstract: The present invention provides a method for the direct esterification of stanols and sterols with fatty acids to form stanol/sterol-esters. The method provides a synthetic route that is amenable to large scale production of the esters in high yields. A preferred embodiment employs a food grade process free of organic solvents or mineral acids, does not produce or use non-food grade products and is substantially free of the use of a catalyst.

Abstract: Certain novel sterol derivatives having no hydroxy group in the 3-position can be used to regulate the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.

Abstract: The present invention relates to novel retinol derivatives having the formula (I): and to processes for preparing them. The invention also relates to the use of these compounds in or for the preparation of compositions intended for treating conditions of the skin or scalp, for example in preventing or combating acne and/or chronological or actinic ageing of the skin.

Abstract: An edible oil is provided that decreases the synthesis, absorption and blood level of cholesterol by a human patient, increases the excretion of cholesterol from the human patient, curtails accumulation of peroxidized material in the blood of the human patient, and also increases the blood level of vitamin E in said human patient.

Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. Further, the culture Fusarium sp., MF6381 (ATCC 74469) is also disclosed, as well as processes for making compounds of structural formula I employing the culture Fusarium sp., MF6381 (ATCC 74469).

Abstract: A method is set forth for separating a sterol or sterol ester from crude tall oil comprising fractionating the crude tall oil into a residue fraction and a volatile fraction, wherein the temperature of the residue fraction does not exceed about 290° C., and wherein the residue fraction includes the sterol or sterol ester. By application of this method, which can be implemented in existing fractionating equipment or in specially designed pitch collecting apparatuses disclosed herein, the yield of sterols can exceed 50% with respect to the sterols present in crude tall oil. A method is also provided for separating unsaponifiable material from a tall oil stream comprising saponifying the stream with a mixture of sodium hydroxide and potassium hydroxide to form sodium and potassium salts of fatty acids, rosin acids, or both; evaporating the unsaponifiable material; and acidulating the unevaporated sodium and potassium salts.

Abstract: Sterols are hydrogenated to stanols in the presence of hydrogenation catalysts in reduced amounts of organic solvent. Both alcohols and paraffin hydrocarbons and also mixtures of alcohols and paraffin hydrocarbons may be used as the solvent. By virtue of the reduced consumption of solvent and the high yield of hydrogenated sterol, the process is particularly suitable for the industrial production of stanols.

Abstract: The invention regards a process for the preparation of a mixture of stanol and stanol fatty acid esters by esterification of phytosterols with a source for fatty acid moieties, in such a way that the degree of esterification of the phytosterols is in the range of 40-85%, and subsequent hardening of the so obtained sterol/sterol fatty acid mixture, the process can be carried out without the use of any solvent, and wherein preferably the fatty acid groups of the stanol fatty acid esters are substantially saturated fatty acid esters. Also claimed are food products comprising mixtures of stanol and stanol fatty acid esters, in particular fat based food products such as yellow fat spreads.

Abstract: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.

Abstract: The present invention pertains to a food ingredient comprising one or more sterols, one or more fats and one or more emulsifiers, as well as to methods of making the food ingredient and food compositions comprising the food ingredient The food ingredient can be used as a cholesterol-lowering agent.

Abstract: A cholesteryl compound has formula (1), and a rewritable full-color thermosensitive recording material contains the above-mentioned cholesteryl compound of formula (1): YO—CO(CH2)n—A—(CH2)nCO—OY  (1) wherein A is a 1,5-hexadienylene group represented by the formula —C(R)═CHCH2CH2CH═C(R)-, in which R is a hydrogen atom or methyl group; Y is a cholesterol residue obtained by removing a hydroxyl group from cholesterol; and n is an integer of 5 to 7.

Abstract: The invention relates to 20-aralkyl-5&agr;-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (H,OR), (H,OSO3H) or NOR; R is H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; X is a straight chain divalent C1-8 hydrocarbon radical, optionally comprising a double or a triple bond; or X is —(CH2)m—CR7R8—; m=0-4; at least one of R7 and R8 is (C1-4)alkyl, hydroxy, (C1-4)alkoxy or halogen; the other, if present, being hydrogen; or R7 and R8 together represent O or NOR′; R′ is H, (C1-6)alkyl or (C1-6)acyl; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR9, R10 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R9 and R10 is independently hydrogen or (C1-4)alkyl; and the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and

Abstract: Fatty acid esters, such as the unsaturated fatty acid esters of sterols and/or stanols, are used as a replacement for a substantial portion or all of the undesirable saturated and trans-unsaturated fats used as structure giving hardstocks in edible foods such as margarines mayonnaise, cooking oils, cheeses, butter and shortening. Because of the similarity in the crystallinity and physical properties of the esters to those of the undesirable hardstock fats, the substitution or replacement contributes favorably to the flavor, texture and other sensory properties of the foods. Only the fatty acid portion of the phytosterol esters defined herein as texturizing agent is digested or absorbed with the sterol part being unabsorbable, thereby resulting in a reduction in total caloric uptake. Furthermore, the phytosterol fatty acid esters reduce the absorption of both dietary and biliary cholesterol from the digestive tract, thereby lowering the blood serum cholesterol level, especially the LDL-cholesterol.